Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Analogues of glucose-dependent insulinotropic polypeptide

an insulinotropic polypeptide and glucose-dependent technology, applied in the field of analogues of glucose-dependent insulinotropic polypeptides, can solve the problems of limited use of unmodified gip as a therapeutic agen

Inactive Publication Date: 2011-06-09
IPSEN PHARMA SAS
View PDF11 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The use of unmodified GIP as a therapeutic, however, is limited by the short in vivo half-life of about 2 minutes (Said and Mutt, 1970, Science, 169:1217-1218).

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Analogues of glucose-dependent insulinotropic polypeptide
  • Analogues of glucose-dependent insulinotropic polypeptide
  • Analogues of glucose-dependent insulinotropic polypeptide

Examples

Experimental program
Comparison scheme
Effect test

example 73

[Aib2, A6c7, Cys(Psu)41]hGIP(1-42)-OH

[0366]Solid-phase peptide synthesis was used to assemble the peptide using microwave-assisted Fmoc Chemistry on a Liberty Peptide Synthesizer (CEM; Matthews, N.C., USA) at the 0.1 mmole scale. Pre-loaded Fmoc-Gln(Trt)-Wang resin (0.59 mmole / g; Novabiochem, San Diego, Calif., USA) was used to generate the C-terminal acid peptide. The resin (0.17 g) was placed in a 50 ml conical tube along with 15 ml of dimethylformamide (DMF) and loaded onto a resin position on the synthesizer. The resin was then quantitatively transferred to the reaction vessel via the automated process. The standard Liberty synthesis protocol for 0.1 mmole scale synthesis was used. This protocol involved deprotecting the N-terminal Fmoc moiety via an initial treatment with 7 ml of 20% piperidine, containing 0.1M N-hydroxybenzotriazole (HOBT), in DMF. The initial deprotection step was for 30 seconds with microwave power (45 watts, maximum temperature of 75° C.), and nitrogen bubb...

example 103

[Orn1(N—C(O)—(CH2)12—CH3), A6c7]hGIP(1-42)-OH

[0369]Solid-phase peptide synthesis was used to assemble the peptide using microwave-assisted Fmoc Chemistry on a Liberty Peptide Synthesizer (CEM; Matthews, N.C., USA) at the 0.1 mmole scale. Pre-loaded Fmoc-Gln(Trt)-Wang resin (0.59 mmole / g; Novabiochem, San Diego, Calif., USA) was used to generate the C-terminal acid peptide. The resin (0.17 g) was placed in a 50 ml conical tube along with 15 ml of dimethylformamide (DMF) and loaded onto a resin position on the synthesizer. The resin was then quantitatively transferred to the reaction vessel via the automated process. The standard Liberty synthesis protocol for 0.1 mmole scale synthesis was used. This protocol involves deprotecting the N-terminal Fmoc moiety via an initial treatment with 7 ml of 20% piperidine, containing 0.1M N-hydroxybenzotriazole (HOBT), in DMF. The initial deprotection step was for 30 seconds with microwave power (45 watts, maximum temperature of 75° C.), and nitro...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Temperatureaaaaaaaaaa
Temperatureaaaaaaaaaa
Temperatureaaaaaaaaaa
Login to View More

Abstract

There is provided a novel series of analogues of glucose-dependent insulinotropic polypeptide compounds, pharmaceutical compositions containing said compounds, and the use of said compounds as GIP-receptor agonists or antagonists for treatment of GIP-receptor mediated conditions, such as non-insulin dependent diabetes mellitus and obesity.

Description

FIELD OF THE INVENTION[0001]The present invention relates to the area of novel analogues of glucose-dependent insulinotropic polypeptide, pharmaceutical compositions containing said compounds, and the use of said compounds as GIP-receptor agonists or antagonists for treatment of GIP-receptor mediated conditions, such as non-insulin dependent diabetes mellitus and obesity.BACKGROUND ART[0002]Glucose-dependent insulinotropic polypeptide (“GIP”, also known as “gastric inhibitory polypeptide”; SEQ ID NO:1) is a 42-residue peptide secreted by enteroendorine K-cells of the small intestine into the bloodstream in response to oral nutrient ingestion. GIP inhibits the secretion of gastric acid, and it has been shown to be a potent stimulant for the secretion of insulin from pancreatic beta cells after oral glucose ingestion (the “incretin effect”) (Creutzfeldt, W., et al., 1979, Diabetologia, 16:75-85).[0003]Insulin release induced by the ingestion of glucose and other nutrients is due to bo...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K38/22C07K14/575A61P5/50A61P3/04A61P3/10A61P3/08A61P3/06A61P1/16A61P19/02A61P19/10A61P3/00A61P25/00A61P25/28A61P13/12A61P9/00A61P9/04A61P11/00A61P9/12
CPCC07K14/605A61K38/00A61P1/16A61P3/00A61P3/04A61P3/06A61P3/08A61P3/10A61P5/48A61P5/50A61P9/00A61P9/04A61P9/10A61P9/12A61P11/00A61P13/12A61P19/02A61P19/08A61P19/10A61P25/00A61P25/28A61P31/10A61P35/00A61P43/00A61K38/28C07K14/62C07K14/645C07K19/00
Inventor DONG, ZHENG XIN
Owner IPSEN PHARMA SAS
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com